Claims
- 1. A peptide analogue suitable as an inhibitor of a prenylpyrophosphate-consuming enzyme complying with formula A-B-B′-D (1):
- 2. The peptide analogue of claim 1, wherein at least one of B and B′ is a residue of an unnatural amino acid.
- 3. The peptide analogue of claim 2, wherein said unnatural amino acid is selected from N-methylglycine, ω-amino C2-8 alkanoic acids and cyclic amino acids.
- 4. The peptide analogue of claim 1, wherein in A Ap is an optionally substituted phenyl group.
- 5. The peptide analogue of claim 1, wherein A is a C12-18 alkanoyl group.
- 6. A peptide analogue suitable as an inhibitor of a prenylpyrophosphate-consuming enzyme complying with formula A-B-B′-D (1):
- 7. The peptide analogue of claim 6, wherein at least one of B and B′ is a residue of an unnatural amino acid.
- 8. The peptide analogue of claim 7, wherein said unnatural amino acid is selected from ω-amino C2-8 alkanoic acids and cyclic amino acids.
- 9. The peptide analogue of claim 6, wherein in D, R5 is selected from piperidino, piperazino, phenyl, nitrophenyl, pyridyl, pyrimidyl, imidazolyl, thiazolyl, naphthyl, quinolyl and indolyl.
- 10. The peptide analogue of claim 9, wherein D is phenylglycine, phenylalanine, nitrophenylalanine, piperidinoalanine, tryptophan, or lysine.
- 11. A method for the treatment of conditions requiring inhibition of the activity of protein:prenyl-transferases or any other prenyl pyrophosphate consuming enzyme, comprising administering a therapeutically effective amount of a peptide analogue according to claim 1.
- 12. The method of claim 11, wherein said conditions comprise osteoporosis, atherosclerosis, restenosis or cancer.
- 13. A pharmaceutical composition containing a peptide analogue according to claim 1, together with a pharmaceutically acceptable carrier.
- 14. A method of assaying protein:prenyl-transferase activity in a biological sample or any other prenyl pyrophosphate consuming enzyme, comprising contacting said sample with a peptide analogue according to claim 1.
- 15. A method for the treatment of conditions requiring inhibition of the activity of protein:prenyl-transferases or any other prenyl pyrophosphate consuming enzyme, comprising administering a therapeutically effective amount of a peptide analogue according to claim 6.
- 16. The method of claim 15, wherein said conditions comprise osteoporosis, atherosclerosis, restenosis or cancer.
- 17. A pharmaceutical composition containing a peptide analogue according to claim 6, together with a pharmaceutically acceptable carrier.
- 18. A method of assaying protein:prenyl-transferase activity in a biological sample or any other prenyl pyrophosphate consuming enzyme, comprising contacting said sample with a peptide analogue according to claim 6.
Priority Claims (1)
Number |
Date |
Country |
Kind |
99203170.8 |
Sep 1999 |
EP |
|
Parent Case Info
[0001] This is a continuation-in-part to U.S. patent application Ser. No. 09/671,298 filed Sep. 28, 2000.
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
09671298 |
Sep 2000 |
US |
Child |
10653069 |
Sep 2003 |
US |